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首页> 外文期刊>Journal of enzyme inhibition >Selective inhibition of monoamine oxidase B by aminoethyl substituted benzyl ethers.
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Selective inhibition of monoamine oxidase B by aminoethyl substituted benzyl ethers.

机译：氨乙基取代的苄基醚对单胺氧化酶B的选择性抑制。

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摘要

Aminoethyl 3-chlorobenzyl ether was shown previously (Ding, C.Z. and Silverman, R.B. (1993). Bioorg. Med. Chem. Lett., 3, 2077-2078) to be a potent and selective time-dependent, but reversible inhibitor of monoamine oxidase B (MAO B). Based on this result, a series of novel aminoethyl substituted benzyl ethers was synthesized and the compounds were examined as potential inhibitors of both isozymic forms of MAO. Each compound in the series inhibits both MAO A and MAO B competitively, and IC50 values for each compound were determined. In general, the B isozyme is much more sensitive to these inhibitors than the A isozyme (except for the o- and p-substituted nitro analogues), in some cases by more than two orders of magnitude. The selectivity in favor of MAO B inhibition is relatively high for all of the meta-substituted analogues and quite low for all of the ortho-substituted analogues. Having the substituent at the ortho-position is most favorable for MAO A inhibition. With MAO B the meta-analogues were, in general, more potent than the corresponding ortho- and para-analogues with respect to their reversible binding constants. The meta-iodo analogue is the most potent analogue.
机译：先前已经证明了氨基乙基3-氯苄基醚（Ding，CZ和Silverman，RB（1993）.Bioorg.Med.Chem.Lett。，3，2077-2078）是有效且选择性的时间依赖性的但可逆的单胺抑制剂。氧化酶B（MAO B）。基于该结果，合成了一系列新颖的氨乙基取代的苄基醚，并检查了该化合物作为MAO的两种同功酶形式的潜在抑制剂。该系列中的每种化合物都竞争性抑制MAO A和MAO B，并确定每种化合物的IC50值。通常，B同工酶对这些抑制剂的敏感性要比A同工酶（除邻位和对位硝基替代物外）更敏感，在某些情况下，其敏感性要高出两个数量级。对于所有间位取代的类似物而言，有利于MAO B抑制的选择性相对较高，而对于所有邻位取代的类似物而言则非常低。在邻位具有取代基对于抑制MAO A是最有利的。就MAO B而言，就其可逆结合常数而言，一般而言，元类似物比相应的邻位和对位类似物更有效。元碘类似物是最有效的类似物。

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